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BDBM426071 4-[2-(4-Fluorophenyl)-3-(1H-indazol-5-yl)imidazo[1,2-a]pyrazin-8-::US10513523, Example 10

SMILES: Fc1ccc(cc1)-c1nc2c(nccn2c1-c1ccc2[nH]ncc2c1)N1CCOCC1

InChI Key: InChIKey=CJGBAZTVYBREGN-UHFFFAOYSA-N

Data: 4 IC50

Find this compound or compounds like it in BindingDB or PDB:
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 4 hits for monomerid = 426071   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kcal/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Glutamate receptor AMPA 1/2


(Homo sapiens (Human))
BDBM426071
PNG
(4-[2-(4-Fluorophenyl)-3-(1H-indazol-5-yl)imidazo[1...)
Show SMILES Fc1ccc(cc1)-c1nc2c(nccn2c1-c1ccc2[nH]ncc2c1)N1CCOCC1
Show InChI InChI=1S/C23H19FN6O/c24-18-4-1-15(2-5-18)20-21(16-3-6-19-17(13-16)14-26-28-19)30-8-7-25-22(23(30)27-20)29-9-11-31-12-10-29/h1-8,13-14H,9-12H2,(H,26,28)
PDB

UniProtKB/SwissProt

antibodypedia
GoogleScholar
AffyNet 
PC cid
PC sid
UniChem
US Patent
n/an/a 0.630n/an/an/an/an/an/a



Janssen Pharmaceutica NV

US Patent


Assay Description
This assay was used to test compounds for their ability to inhibit TARP γ8 dependent AMPA receptor activity. The AMPA receptor is a non-selectiv...


US Patent US10513523 (2019)


BindingDB Entry DOI: 10.7270/Q2KW5JDR
More data for this
Ligand-Target Pair
Cytochrome P450 2C9


(Homo sapiens (Human))
BDBM426071
PNG
(4-[2-(4-Fluorophenyl)-3-(1H-indazol-5-yl)imidazo[1...)
Show SMILES Fc1ccc(cc1)-c1nc2c(nccn2c1-c1ccc2[nH]ncc2c1)N1CCOCC1
Show InChI InChI=1S/C23H19FN6O/c24-18-4-1-15(2-5-18)20-21(16-3-6-19-17(13-16)14-26-28-19)30-8-7-25-22(23(30)27-20)29-9-11-31-12-10-29/h1-8,13-14H,9-12H2,(H,26,28)
PDB
MMDB

Reactome pathway
KEGG

UniProtKB/SwissProt
UniProtKB/TrEMBL

B.MOAD
DrugBank
antibodypedia
GoogleScholar
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PC cid
PC sid
UniChem
Article
PubMed
n/an/a 500n/an/an/an/an/an/a



Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL


Assay Description
Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate measured after 15 mins in presence of NADPH by LC-MS/MS analysis


ACS Med Chem Lett 10: 267-272 (2019)


Article DOI: 10.1021/acsmedchemlett.8b00599
More data for this
Ligand-Target Pair
GRIA1/CACNG2


(Homo sapiens (Human))
BDBM426071
PNG
(4-[2-(4-Fluorophenyl)-3-(1H-indazol-5-yl)imidazo[1...)
Show SMILES Fc1ccc(cc1)-c1nc2c(nccn2c1-c1ccc2[nH]ncc2c1)N1CCOCC1
Show InChI InChI=1S/C23H19FN6O/c24-18-4-1-15(2-5-18)20-21(16-3-6-19-17(13-16)14-26-28-19)30-8-7-25-22(23(30)27-20)29-9-11-31-12-10-29/h1-8,13-14H,9-12H2,(H,26,28)
PDB

UniProtKB/SwissProt

antibodypedia
GoogleScholar
AffyNet 
PC cid
PC sid
UniChem
Article
PubMed
n/an/a 0.631n/an/an/an/an/an/a



Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL


Assay Description
Negative allosteric modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293 cells assessed as inhibition of glutamate-induc...


ACS Med Chem Lett 10: 267-272 (2019)


Article DOI: 10.1021/acsmedchemlett.8b00599
More data for this
Ligand-Target Pair
Voltage-dependent calcium channel gamma-8 subunit


(Rattus norvegicus)
BDBM426071
PNG
(4-[2-(4-Fluorophenyl)-3-(1H-indazol-5-yl)imidazo[1...)
Show SMILES Fc1ccc(cc1)-c1nc2c(nccn2c1-c1ccc2[nH]ncc2c1)N1CCOCC1
Show InChI InChI=1S/C23H19FN6O/c24-18-4-1-15(2-5-18)20-21(16-3-6-19-17(13-16)14-26-28-19)30-8-7-25-22(23(30)27-20)29-9-11-31-12-10-29/h1-8,13-14H,9-12H2,(H,26,28)
PDB
MMDB

NCI pathway
Reactome pathway
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DrugBank
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PC cid
PC sid
UniChem
Article
PubMed
n/an/a<1.00E+4n/an/an/an/an/an/a



Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL


Assay Description
Negative allosteric modulation of TARPgamma8 in rat hippocampal neurons assessed as inhibition of glutamate-induced current at 10 uM at -60 mV holdin...


ACS Med Chem Lett 10: 267-272 (2019)


Article DOI: 10.1021/acsmedchemlett.8b00599
More data for this
Ligand-Target Pair